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Methods for treating resistant diseases using triazole containing macrolides

a triazole and macrolide technology, applied in the field of resistant diseases, can solve the problems of limited clinical utility of this drug, inactiveness, and increased risk of pneumonia causing community-acquired respiratory infection, and achieve low resistance development potential, high activity in vitro and in vivo, and low potential

Inactive Publication Date: 2011-08-18
TETARD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The patent text describes a new group of antibiotics called triazole-containing macrolides, which are effective against resistant bacteria. These compounds have a low potential for resistance development and are currently being tested in clinical trials. The technical effect of this discovery is that it provides a new tool for treating drug-resistant bacteria, which is becoming a serious problem worldwide."

Problems solved by technology

Further, TEL is not active against erm(B) group A streptococci (which are naturally TEL resistant).
Moreover, observed TEL toxicities have limited the clinical utility of this drug.
Thus, the problem of drug-resistant pneumococci causing community-acquired respiratory infection, especially in children, is likely to worsen with the spread of this clone.
Further, those new agents would desirably have the property of a low potential for resistance development or induction, and a low potential for naturally occurring resistance.

Method used

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  • Methods for treating resistant diseases using triazole containing macrolides
  • Methods for treating resistant diseases using triazole containing macrolides
  • Methods for treating resistant diseases using triazole containing macrolides

Examples

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[0202]Staphylococci, β-Haemolytic and Viridans Group Streptococci. A collection of 2006-2007 clinical isolates were S tested by CLSI methods (M7-A7) with associated interpretive criteria (M100-S18) and supplements (2-5% LHB) for streptococcal tests. CEM-101, TEL (TEL) and 10 comparators were used versus 201 S. aureus (75 WT-MRSA, 75 WT-MSSA, 30 CA-MRSA, 17 VISA or hVISA, 7 VRSA), 100 coagulase-negative staphylococci (CoNS; 10 species), 100 β-haemolytic (BHS; 30 group A, 31 group B, 14 group C, 9 group F, 16 group G) and 51 viridans group streptococci (VGS; 5 species), see Table.

[0203]MSSA strains were slightly more CEM-101-S (MIC50, 0.06 μg / ml) that MRSA or CA-MRSA strains (MIC50, 0.12 μg / ml). VISA, hVISA and VRSA were generally more refractory to CEM-101 and TEL. CEM-101 was 2-fold more potent than TEL against all staphylococci. Streptococci were very S to CEM-101 (MIC90, 0.03-0.06 μg / ml) and TEL was 4-fold less active with non-S isolates of BHS observed. ERY-R staphylococci remain...

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Abstract

Triazole-containing macrolide and ketolide antibiotics, therapeutic compositions containing them and methods of use for treating diseases caused by one or more resistant organisms are described.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority under 35 USC §119(e) to U.S. Provisional Application Ser. No. 61 / 108,110, filed on Oct. 24, 2008, U.S. Provisional Application Ser. No. 61 / 108,112, filed on Oct. 24, 2008, U.S. Provisional Application Ser. No. 61 / 108,134, filed on Oct. 24, 2008, U.S. Provisional Application Ser. No. 61 / 108,137, filed on Oct. 24, 2008, U.S. Provisional Application Ser. No. 61 / 108,168, filed on Oct. 24, 2008, and U.S. Provisional Application Ser. No. 61 / 162,109, filed on Mar. 20, 2009, the entire disclosure of each of which are incorporated herein by reference.TECHNICAL FIELD[0002]The invention described herein relates to the treatment of resistant diseases, or more particularly, diseases caused at least in part by one or more resistant organisms. In particular, the invention described herein relates to the treatment of resistant diseases, or more particularly, diseases caused at least in part by one or more resistant organi...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/7056A61P31/04
CPCA61K31/70A61K31/7056A61K31/706A61K31/7048A61K31/7052A61K31/424C07D498/04C07H17/08A61P1/00A61P1/04A61P11/00A61P29/00A61P31/00A61P31/04A61P33/02Y02A50/30
Inventor FERNANDES, PRABHAVATHI B.PEREIRA, DAVID E.
Owner TETARD INC
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